1. Field of the Invention
This invention is directed to a novel method for relieving, inhibiting or preventing ophthalmic diseases caused by or associated with increased intraocular pressure. The method is particularly useful in the number of clinical cases included in the category of glaucoma.
Compound .+-.2-[(3,4-methylenedioxy)phenethyl]-5-[(3-carboxamido-4-hydroxy)-.alpha. -hydroxybenzyl]pyrrolidine, any of its stereoisomers and their pharmaceutically acceptable acid addition salts have been shown to lower intraocular pressure in mammals and are, therefore, useful in the treatment of all ophthalmic diseases which profess the increased intraocular pressure. Although these compounds are particularly useful in treatment of glaucoma, the other ophthalmic diseases which are accompanied with or caused by increased intraocular pressure will also respond to the treatment.
Compounds of this invention profess several advantages over existing treatment of intraocular pressure. They are non-irritating to the eye, they have long lasting activity, they do not show contralateral effect, they lack systemic activity, and they are as, or more, effective than labetolol or timolol, a known intraocular pressure lowering agent.
2. Related Disclosures
Attempts to find effective treatment of ocular hypertension are known. Catecholamine treatment of ocular hypertension is described in U.S. Pat. No. 4,275,074. Treating glaucoma and lowering intraocular pressure by topical administration of R,R-labetolol is described in U.S. Pat. No. 4,312,863. Reducing intraocular pressure in glaucomatous dogs with N-demethylated carbachol is described in Invest. Ophthalmic Vis. Sci., 19:1198 (1980). U.S. Pat. No. 4,322,425 describes an ophthalmic composition containing a carbostyril derivative useful for treatment of glaucoma.
The compounds of this invention are the subject of the currently pending patent applications Ser. No. 460,204 and Ser. No. 527,716 describing their systemic hypotensive effect. These compounds were not previously administered topically, i.e., directly to the eye, to prevent, inhibit or treat ophthalmic diseases because their non-irritating properties to the eye were unknown, and are unexpected and surprising.